The objective of this research is to synthesize and screen in standard antitumor assays new analogs of the mitomycins. Design of these analogs is based upon the mechanism of action of the mitomycins and those structure-activity relationships presently known. It is hoped that clinical agents superior to mitomycin C can be prepared. For the synthesis of analogs, efficient sequencces are being developed. These sequences lead through certain key intermediates, from which relatively large numbers of analogs can be prepared by a few steps each. Antitumor assays will be conducted by the CCNSC and at Bristol Laboratories. BIBLIOGRAPHIC REFERENCES: Synthesis and Biological Activity of a 1,2-Disubstituted-7-methoxymitosene, W.G. Taylor, D.L. Fost, G. Leadbetter, and W.A. Remers, J. Med. Chem., 20, 138(1977). Comparative Stereochemistry in the Aziridine Ring Openings of N-Methyl-mitomycin A and 7- Methoxy-1,2-(N-methylaziridino)-mitosene, L. Cheng and W.A. Remers, J. Med. Chem., in press (June, 1977).